EP2321302A4 - Azacitidine process and polymorphs - Google Patents

Azacitidine process and polymorphs

Info

Publication number
EP2321302A4
EP2321302A4 EP09803639A EP09803639A EP2321302A4 EP 2321302 A4 EP2321302 A4 EP 2321302A4 EP 09803639 A EP09803639 A EP 09803639A EP 09803639 A EP09803639 A EP 09803639A EP 2321302 A4 EP2321302 A4 EP 2321302A4
Authority
EP
European Patent Office
Prior art keywords
azacitidine
polymorphs
azacitidine process
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP09803639A
Other languages
German (de)
French (fr)
Other versions
EP2321302A2 (en
EP2321302B1 (en
Inventor
Praveen Cherukupally
Satish Kumar Vujjini
Ganesh Varanasi
Sreenadha Charyulu Kandala
Srinivas Areveli
Satyanarayana Raju Tirumalaraju
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dr Reddys Laboratories Ltd
Dr Reddys Laboratories Inc
Original Assignee
Dr Reddys Laboratories Ltd
Dr Reddys Laboratories Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41610970&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP2321302(A4) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Dr Reddys Laboratories Ltd, Dr Reddys Laboratories Inc filed Critical Dr Reddys Laboratories Ltd
Publication of EP2321302A2 publication Critical patent/EP2321302A2/en
Publication of EP2321302A4 publication Critical patent/EP2321302A4/en
Application granted granted Critical
Publication of EP2321302B1 publication Critical patent/EP2321302B1/en
Revoked legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/12Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group -X-C(=X)-X-, or halides thereof, in which each X means nitrogen, oxygen, sulfur, selenium or tellurium, e.g. carbonic acid, carbamic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12Triazine radicals
EP09803639.5A 2008-08-01 2009-07-31 Azacitidine process and polymorphs Revoked EP2321302B1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN1854CH2008 2008-08-01
US10206408P 2008-10-02 2008-10-02
IN3053CH2008 2008-12-03
US15417109P 2009-02-20 2009-02-20
PCT/US2009/052376 WO2010014883A2 (en) 2008-08-01 2009-07-31 Azacitidine process and polymorphs

Publications (3)

Publication Number Publication Date
EP2321302A2 EP2321302A2 (en) 2011-05-18
EP2321302A4 true EP2321302A4 (en) 2011-12-21
EP2321302B1 EP2321302B1 (en) 2014-10-29

Family

ID=41610970

Family Applications (1)

Application Number Title Priority Date Filing Date
EP09803639.5A Revoked EP2321302B1 (en) 2008-08-01 2009-07-31 Azacitidine process and polymorphs

Country Status (3)

Country Link
US (2) US8703932B2 (en)
EP (1) EP2321302B1 (en)
WO (1) WO2010014883A2 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6943249B2 (en) * 2003-03-17 2005-09-13 Ash Stevens, Inc. Methods for isolating crystalline Form I of 5-azacytidine
US6887855B2 (en) * 2003-03-17 2005-05-03 Pharmion Corporation Forms of 5-azacytidine
EP3782611B1 (en) * 2008-05-15 2022-07-06 Celgene Corporation Oral formulations of cytidine analogs and methods of use thereof
WO2010014883A2 (en) * 2008-08-01 2010-02-04 Dr. Reddy's Laboratories Ltd. Azacitidine process and polymorphs
JP5650643B2 (en) 2008-08-08 2015-01-07 サイノファーム タイワン リミテッド Method for producing 5-azacytosine nucleoside and derivatives thereof
AR076418A1 (en) * 2009-04-27 2011-06-08 Reddys Lab Inc Dr DECITABIN PREPARATION
CN101974051B (en) * 2010-10-08 2012-08-08 重庆泰濠制药有限公司 Method for synthesizing azacitidine
JP6289361B2 (en) 2011-03-31 2018-03-07 セルジーン インターナショナル サルル Synthesis of 5-azacytidine
CN103254145B (en) * 2013-05-14 2015-04-08 同济大学 Method for synthesizing nanoscale melamine phosphate by hydrothermal method
CN103450303A (en) * 2013-09-04 2013-12-18 重庆泰濠制药有限公司 Azacitidine crystal form A and azacitidine crystal form B as well as preparation method thereof
CA2963686A1 (en) 2014-10-08 2016-04-14 Epigenetics Pharma Llc Silylated pyrimidine prodrugs and methods of their use
CN104402836B (en) * 2014-11-04 2016-06-08 常州康丽制药有限公司 The preparation method of 5-azepine cytosine
CN105837524B (en) * 2016-04-28 2018-07-20 宁夏思科达生物科技有限公司 A kind of synthetic method of 5- azepines cytimidine
CN109651451B (en) * 2017-10-10 2023-07-11 芜湖先声中人药业有限公司 Azacitidine derivative preparation method and application thereof
CN110092807A (en) * 2018-01-30 2019-08-06 中国医学科学院药物研究所 A kind of method for preparing azacitidine of high-purity, low ignition residue
CN109020907B (en) * 2018-09-07 2022-02-01 山东第一医科大学(山东省医学科学院) Novel synthesis method of 5-azacytosine
CN112279881A (en) * 2020-10-12 2021-01-29 福建南方制药股份有限公司 Method for preparing antitumor drug azacitidine
CN112300222B (en) * 2020-11-26 2023-03-21 北京益佰医药研究有限公司 Azacitidine refining method with high purity and low solvent residue

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4082911A (en) * 1975-02-24 1978-04-04 Schering Aktiengesellschaft Process for the preparation of nucleosides
US4209613A (en) * 1977-12-20 1980-06-24 Schering Aktiengesellschaft Process for the preparation of nucleosides

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1050899A (en) 1963-12-22
DE2012888C3 (en) 1970-03-14 1981-04-02 Schering Ag, 1000 Berlin Und 4619 Bergkamen Process for the preparation of 5-azapyrimidine nucleosides
US3819780A (en) 1971-01-05 1974-06-25 N Anderson Injection molding of nylon foam panels
US6943249B2 (en) 2003-03-17 2005-09-13 Ash Stevens, Inc. Methods for isolating crystalline Form I of 5-azacytidine
US7038038B2 (en) * 2003-03-17 2006-05-02 Pharmion Corporation Synthesis of 5-azacytidine
US6887855B2 (en) 2003-03-17 2005-05-03 Pharmion Corporation Forms of 5-azacytidine
US7192781B2 (en) * 2004-04-13 2007-03-20 Pharmion Corporation Methods for stabilizing 5-azacytidine in plasma
UA99308C2 (en) * 2007-09-26 2012-08-10 Маунт Синай Скул Оф Медсин Azacytidine analogue and use thereof
WO2010014883A2 (en) * 2008-08-01 2010-02-04 Dr. Reddy's Laboratories Ltd. Azacitidine process and polymorphs

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4082911A (en) * 1975-02-24 1978-04-04 Schering Aktiengesellschaft Process for the preparation of nucleosides
US4209613A (en) * 1977-12-20 1980-06-24 Schering Aktiengesellschaft Process for the preparation of nucleosides

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2010014883A2 *

Also Published As

Publication number Publication date
EP2321302A2 (en) 2011-05-18
WO2010014883A3 (en) 2010-05-14
WO2010014883A2 (en) 2010-02-04
US9416152B2 (en) 2016-08-16
US8703932B2 (en) 2014-04-22
EP2321302B1 (en) 2014-10-29
US20140155588A1 (en) 2014-06-05
US20110201800A1 (en) 2011-08-18

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